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去甲氧基姜黄酮（一种来自[具体来源未给出]的次生代谢产物）与人单胺氧化酶-A和氧化酶-B的相互作用。

Interactions of Desmethoxyyangonin, a Secondary Metabolite from , with Human Monoamine Oxidase-A and Oxidase-B.

作者信息

Chaurasiya Narayan D, León Francisco, Ding Yuanqing, Gómez-Betancur Isabel, Benjumea Dora, Walker Larry A, Cutler Stephen J, Tekwani Babu L

机构信息

National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.

Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.

出版信息

Evid Based Complement Alternat Med. 2017;2017:4018724. doi: 10.1155/2017/4018724. Epub 2017 Aug 24.

DOI:10.1155/2017/4018724
PMID:29138643
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5613693/
Abstract

(Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites and other injuries and also as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of leaves showed potent inhibition of human monoamine oxidases- (MAOs-) A and B. Phytochemical studies yielded six known compounds, including pinostrobin , 4'-methyl ether sakuranetin , sakuranetin , pinostrobin chalcone , yashabushidiol A , and desmethoxyyangonin . Compound displayed about 30-fold higher affinity for MAO-B than MAO-A, with Ki values of 31 and 922 nM, respectively. Kinetic analysis of inhibition and equilibrium-dialysis dissociation assay of the enzyme-inhibitor complex showed reversible binding of desmethoxyyangonin with MAO-A and MAO-B. The binding interactions of compound in the active site of the MAO-A and MAO-B isoenzymes, investigated through molecular modeling algorithms, confirmed preferential binding of desmethoxyyangonin with MAO-B compared to MAO-A. Selective reversible inhibitors of MAO-B, like desmethoxyyangonin may have important therapeutic significance for the treatment of neurodegenerative disorders, such as Parkinson's disease and Alzheimer's disease.

摘要

（姜科）是一种热带雨林药用植物，用于治疗蛇咬伤和其他损伤，还用作退烧药、镇痛药、止吐药、抗溃疡药和抗惊厥药。该植物叶片的二氯甲烷提取物对人单胺氧化酶 -（MAOs-）A和B显示出强效抑制作用。植物化学研究得到了六种已知化合物，包括豆甾酮、4'-甲基醚樱花素、樱花素、豆甾酮查耳酮、矢车菊二醇A和去甲氧基姜黄酮。化合物对MAO - B的亲和力比对MAO - A高约30倍，其Ki值分别为31和922 nM。抑制动力学分析和酶 - 抑制剂复合物的平衡透析解离试验表明，去甲氧基姜黄酮与MAO - A和MAO - B的结合是可逆的。通过分子模拟算法研究了该化合物在MAO - A和MAO - B同工酶活性位点的结合相互作用，证实去甲氧基姜黄酮与MAO - B的结合比与MAO - A更具选择性。像去甲氧基姜黄酮这样的MAO - B选择性可逆抑制剂可能对治疗神经退行性疾病如帕金森病和阿尔茨海默病具有重要的治疗意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/af0748065a8d/ECAM2017-4018724.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/8667c26fd231/ECAM2017-4018724.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/297e034612b0/ECAM2017-4018724.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/3df7b8acfe5d/ECAM2017-4018724.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/140cdb7ca47d/ECAM2017-4018724.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/c941d0e8af34/ECAM2017-4018724.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/3d48aefa46ab/ECAM2017-4018724.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/af0748065a8d/ECAM2017-4018724.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/8667c26fd231/ECAM2017-4018724.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/297e034612b0/ECAM2017-4018724.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/3df7b8acfe5d/ECAM2017-4018724.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/140cdb7ca47d/ECAM2017-4018724.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/c941d0e8af34/ECAM2017-4018724.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/3d48aefa46ab/ECAM2017-4018724.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac9f/5613693/af0748065a8d/ECAM2017-4018724.007.jpg

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